Regulated protonation of polyaspartamide derivatives bearing repeated aminoethylene side chains for efficient intracellular siRNA delivery with minimal cytotoxicity.
نویسندگان
چکیده
The effects of the repeated number (RN) of aminoethylene (AE) units in polyaspartamide side chains were investigated for polyion complex (PIC)-based siRNA delivery. Reduction of the apparent RN from 3 to 2 by thiourea introduction increased a protonatable amine fraction in AE units at endosomal pH, leading to the efficient endosomal escape of siRNA-loaded PICs.
منابع مشابه
Introduction of stearoyl moieties into a biocompatible cationic polyaspartamide derivative, PAsp(DET), with endosomal escaping function for enhanced siRNA-mediated gene knockdown.
Applications of siRNA for cancer therapy have been spotlighted in recent years, but the rational design of efficient siRNA delivery carriers is still controversial, especially because of possible toxicity of the carrier components. Previously, a cationic polyaspartamide derivative, poly{N-[N-(2-aminoethyl)-2-aminoethyl]aspartamide} (PAsp(DET)), was reported to exert high transfection efficacy f...
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عنوان ژورنال:
- Chemical communications
دوره 51 15 شماره
صفحات -
تاریخ انتشار 2015